Electrochemical polymerization of 3-phenylthiophene

Poly (3-phenylthiophene) (P3PhT) films have been electrochemically synthesized by direct oxidation of 3-phenylthiophene in the electrolyte of pure boron trifluoride diethyl etherate (BFEE). The oxidation potential of the monomer was measured to be 1.29 V (vs. SCE), and about 0.15 V lower than that measured in a neutral medium of acetonitrile. Free-standing P3PhT film with tensile strength of 32–40 MPa has been obtained for the first time. The morphology and the structure of the polymer film have been studied by scanning electron microscopy, infrared and Raman spectroscopies. Raman spectral results demonstrated that the doping level of the P3PhT film increased with film thickness during electrochemical growth process.     

拮氟锐对大鼠肠道氟吸收及微量元素的影响

拮氟锐是由硼、微量元素和中药制成的抗氟药物。本文应用肠道原位灌流技术。观察了拮氟锐对大鼠肠道氟吸收的干预作用及微量元素的影响。结果透明：拮氟锐可促进肠道ＢＦ４的形成，使氟吸收量减少，血氟降低。同时，拮氟锐可拮抗氟所致的微量元素的降低。与硼锌组比较，拮氟锐的抗氟作用效果更明显。     

极谱配合物吸附波测定人发中硼

目的：探讨在ｐＨ４．４乙酸－乙酸钠－ＥＤＴＡ－铍试剂Ⅲ底液中用极谱配合物吸附波测定人发中硼。方法：极谱法。结果：线性范围为３．７×１０－７ｍｏｌ／Ｌ～１．８×１０－５ｍｏｌ／Ｌ,变异系数为５．５％～７．４％,样品加标回收率为９２．８％～９８．０％。结论：本法简便快速,灵敏度高,选择性好。     

A targeting model of boron neutron-capture therapy to hepatoma cellsin vivo with a boronated anti-(α-fetoprotein) monoclonal antibody

We described previously that¹⁰B atoms delivered by monoclonal antibody (mAb) exerted a cytotoxic effect on AH66 cells in a dose-dependent manner upon thermal neutron irradiationin vitro. In the present study, the delivering capacity of boronated anti-(-fetoprotein) (AFP) mAb to carry¹⁰B atoms to AFP-producing tumor xenografts in nude mice was determined. Boronated mAb was prepared by conjugating 50 mM ¹⁰B compound to an anti-AFP mAb (2 mg/ml) usingN-succinimidyl-3-) (2-pyridyldithio) propionate. The number of¹⁰B atoms conjugated directly to the mAb was estimated to be 459/antibody by prompt -ray spectrometry. Boron concentrations in tumor tissue obtained 12, 24, 72, and 120 h after injection of 3.0 mg¹⁰B-conjugated anti-AFP mAb were 11.10±3.12 (SD,n=6), 29.30±5.11, 33.02±11.8, and 12.91±5.62 ppm respectively. For control¹⁰B-conjugated anti-dinitrophenol (DNP) mAb, the values were 9.59±0.99, 10.37±2.86, 10.00±2.95, and 8.83±4.71 ppm respectively. The concentrations in blood were less than 0.40±0.10 ppm with anti-AFP mAb and less than 0.51±0.15 ppm with anti-DNP mAb at each sampling time (12, 24, 72, and 120 h). The number of¹⁰B atoms delivered to the tumor cells was calculated to be 0.62×10⁹, 1.63×10⁹, 1.84×10⁹ and 0.72×10⁹ at each sampling time after injection of¹⁰B-anti-AFP mAb. The amount of¹⁰B atoms necessary for effective boron neutron-capture therapy was estimated to be 10⁹/tumor cell. We were able to carry 1.84×10^{9 10}B atoms to AH66 tumor cells by using¹⁰B-anti-AFP mAb. The accumulation reached its peak 72 h after injection. These data indicated that the¹⁰B-conjugated antitumor mAb could deliver a sufficient amount of¹⁰B atoms to the tumor cells to induce cytotoxic effects 72 h after injection upon thermal neutron irradiation.Abbreviations BNCT boron neutron-capture therapy - AFP -fetoprotein - SPDP N-succinimidyl-3-(2-pyridyldithia) propionate - DNP dinitrophenol     

Improved Stability and Practicality for Synthesis of 4-Borono-2-[18F]fluoro-l-phenylalanine by Combination of [18O]O2 Single-Use and [18F]CH3COOF Labeling Agents

Purpose4-Borono-2-[¹⁸F]fluoro-l-phenylalanine ([¹⁸F]FBPA) synthesized with [¹⁸F]F₂, produced using the ¹⁸O(p, n)¹⁸F reaction, has been reported for increasing radioactivity. However, a dedicated system and complex procedure is required to reuse the costly [¹⁸O]O₂ gas; also, the use of [¹⁸F]F₂ as a labeling agent reduces the labeling rate and radiochemical purity. We developed a stable and practical method for [¹⁸F]FBPA synthesis by combining [¹⁸F]F₂, produced using a [¹⁸O]O₂ single-use system, and a [¹⁸F]CH₃COOF labeling agent.MethodsThe produced [¹⁸F]F₂ was optimized, and then [¹⁸F]FBPA was synthesized. For passivation of the target box, 0.5% F₂ was pre-irradiated in argon. Gaseous products were discarded; the target box was filled with [¹⁸O]O₂ gas, and then irradiated (first irradiation). Then, the [¹⁸O]O₂ gas was discarded, 0.05–0.08% F₂ in argon was fed into the target box, and it was again irradiated (second irradiation). The [¹⁸F]F₂ obtained after this was passed through a CH₃COONa column, converting it into the [¹⁸F]CH₃COOF labeling agent, which was then used for [¹⁸F]FBPA synthesis.ResultsThe mean amount of as-obtained [¹⁸F]F₂ was 55.0 ± 3.3 GBq and that of as-obtained [¹⁸F]CH₃COOF was 21.6 ± 1.4 GBq after the bombardment. The radioactivity and the radiochemical yield based on [¹⁸F]F₂ of [¹⁸F]FBPA were 4.72 ± 0.34 GBq and 12.2 ± 0.1%, respectively. The radiochemical purity and molar activity were 99.3 ± 0.1% and 231 ± 22 GBq/mmol, respectively.ConclusionWe developed a method for [¹⁸F]FBPA production, which is more stable and practical compared with the method using [¹⁸O]O₂ gas-recycling and [¹⁸F]F₂ labeling agent.     

硼、镁较优抗氟剂量的确定及联合应用预防小鼠氟牙症的研究

目的：通过在食物中添加微量元素镁、硼,观察小鼠氟斑牙的减轻程度,进一步确定镁、硼元素抗氟的较优剂量,并进行两种元素较优剂量的联合应用。方法：120只雄性ICR小鼠,随机分为12组,空白组饮用双蒸水,加氟组饮用含NaF110 mg／L的双蒸水,均进食普通饲料。镁、硼元素组分别将四硼酸钠（ Na2 B4 O7?10 H2 O）、硫酸镁（ MgSO4?7 H2 O）按照不同的剂量添加于饲料中,饮水同加氟组。实验期间观察小鼠体重及牙长增长率,氟斑牙的形成时间、形成分级及第42 d（ D42）分级,将镁、硼元素抗氟的较优剂量组联合应用,观察其抗氟效果。结果：四硼酸钠878．55 mg／kg饲料和硫酸镁162．5 mg／kg饲料组氟斑牙形成的时间、形成分级和D42分级均小于加氟组及其它剂量组（P＜0．05）,以四硼酸钠878．55 mg／kg饲料组为单独使用抗氟元素的最优剂量。结论：硫酸镁162．5 mg／kg饲料为镁元素实验组的较优剂量,四硼酸钠878．55 mg／kg饲料为整个实验组的最优剂量。硼镁较优剂量组联用的抗氟效果不及四硼酸钠878．55 mg／kg饲料剂量组。     

硼中子俘获治疗对裸鼠脏器影响的实验研究

目的采用动物实验方法研究硼中子俘获疗法(BNCT)对于正常脏器的损伤作用,从而为其安全性研究提供依据。方法实验动物裸小鼠随机分成单纯照射中子组(Ⅰ组),单纯给药组(Ⅱ组),BNCT 1、2、3组(Ⅲ、Ⅳ、Ⅴ组)。其中BNCT 1组为注射硼携带剂BPA(300 mg/kg,B.W.)2.5 h后接受超热中子束满功率照射10 min,BNCT 2组为注射硼携带剂BPA(500 mg/kg,B.W.)2.5 h后接受超热中子束满功率照射10 min,BNCT 3组为注射硼携带剂BPA(300 mg/kg,B.W.)2.5 h后接受超热中子束满功率照射15 min。实验完成后2周处理动物,将各组动物脏器心、肺、肝、脾、肾、膀胱切取后HE染色,病理切片,两名经验丰富的病理科医师观察脏器淤血,水肿,坏死,增生情况。结果将各组数据统计学处理采用等级计数资料的Ridit分析。结果显示各组心、肺、脾、肾、膀胱损伤及肝细胞坏死及非典型增生差异无统计学意义,肝组织淤血、水样变性实验组损伤小于对照组,差异有统计学意义。结论 BNCT对裸鼠脏器损伤小,是一项安全的治疗方法,为进一步用BNCT治疗肿瘤提供了依据。     

硼中子俘获治疗的加速器中子源7Li(p,n)7Be的中子特性研究

目的 通过研究质子加速器 ⁷Li(p,n)⁷Be 反应的中子特性,为研究和制作适用于硼中子俘获治疗(BNCT)的加速器中子源提供基础数据。方法 加速质子使其轰击Li靶后产生中子;通过金属箔活化法,测量中子与In箔发生阈值反应后放出的γ射线;然后计算出In箔的放射性活度、加速器反应后放出中子的注量和反应的微分截面。结果 质子加速轰击Li靶后,在不同方向产生不同能量和注量的中子。加速器电压分别为3.0、2.8和2.6 MV,出射中子与入射质子束的方向一致时, ⁷Li(p,n)⁷Be 反应的微分截面约为50 mb/mr;夹角为60°时,反应的微分截面减小到30 mb/mr左右。由于部分中子与其他金属原子等发生弹性散射而射向后方,提高了这一范围内In箔的比放射性活度,影响了其微分截面的准确性。结论 用金属箔活化法测定中子简便易行,可同时测得多个方向的中子分布,但需对中子与其他金属弹性散射产生的影响进行进一步的研究; ⁷Li(p,n)⁷Be 反应后发射出的中子经慢化后,能得到适于BNCT治疗的热中子和超热中子;若作为BNCT的中子源,加速器的质子束流需达到10 mA。     

胶质瘤细胞系摄取BPA实验研究

目的　探讨孵育时间和细胞周期对胶质瘤细胞摄取BPA(p boronophenylalanine)的影响 ,进一步阐明BPA的胶质瘤细胞选择性作用机制。方法　将C6 ,BT 32 5 ,SHG 4 4胶质瘤细胞和原代大鼠星形胶质细胞培养在含BPA的培养液中 ,分别培养 4h、8h、12h、16h、2 0h和 2 4h后 ,采用感应耦合等离子体原子发射光谱 (ICP AES)法测定细胞内硼的含量。培养 2 4h后 ,流式细胞仪分选G0 /G1和G2 /M期的细胞 ,ICP AES法分别测定细胞内硼的水平。结果　三种胶质瘤细胞在每个检测时间点的细胞内硼含量均显著高于对照组胶质细胞 (P <0 .0 1)。三种胶质瘤细胞G2 /M期与G0 /G1期相比硼含量均明显增高 (P <0 .0 5 ) ,而星形胶质细胞两期差异不明显。C6、SHG 4 4和BT 32 5与星形胶质细胞G0 /G1期的硼浓度比分别为 1.4 6、1.5 1和 1.4 0 ,G2 /M期的硼浓度比分别为 3.6 5、3.96和3.76。结论　有丝分裂的过程可以加强胶质瘤对BPA的吸收 ,这一过程可能与胶质瘤细胞对BPA的主动运输有关。主动运输可能是BPA对胶质瘤选择性作用的基础